[go: up one dir, main page]

PE20100741A1 - COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38 - Google Patents

COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38

Info

Publication number
PE20100741A1
PE20100741A1 PE2010000198A PE2010000198A PE20100741A1 PE 20100741 A1 PE20100741 A1 PE 20100741A1 PE 2010000198 A PE2010000198 A PE 2010000198A PE 2010000198 A PE2010000198 A PE 2010000198A PE 20100741 A1 PE20100741 A1 PE 20100741A1
Authority
PE
Peru
Prior art keywords
pyrimidin
dihydropyrimide
kinase inhibitors
compounds derived
tetrahydropyrimido
Prior art date
Application number
PE2010000198A
Other languages
Spanish (es)
Inventor
James Francis Callahan
Zehong Wan
Hongxing Yan
Original Assignee
Glaxo Group Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE20100741A1 publication Critical patent/PE20100741A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA 1, DONDE R1 ES DE PREFERENCIA -C(O)N-CH(CH3)-CH3, C(O)NCH2-CH2-CH3, ENTRE OTROS; R1' ES HALOGENO, ALQUILO C1-4 SUSTITUIDO O NO CON HALO. CIANO, NITRO, ENTRE OTROS; G1 Y G2 SON INDEPENDIENTEMENTE NITROGENO; G3 ES NH; R3 ES FENILO OPCIONALMENTE SUSTITUIDO UNA O MAS VECES CON HALOGENO, NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-[2-(4-AMINO-1-PIPERIDINIL)-8-(2,6-DIFLUOROFENIL)-7-OXO-5,6,7,8-TETRAHIDROPIRIMIDO[4,5-d]PIRIMIDIN-4-IL]-N-CICLOBUTIL-4-METILBENZAMIDA; 3-{8-(2,6-DIFLUOROFENIL)-2-[[3-(DIMETILAMINO)PROPIL](METIL)AMINO]-7-OXO-5,6,7,8-TETRAHIDROPIRIMIDO[4,5-d]PIRIMIDIN-4-IL}-4-METIL-N-(FENILMETIL)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE CINASAS CSBP/p38/RK UTIL EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIASREFERS TO A COMPOUND OF FORMULA 1, WHERE R1 IS PREFERRED -C (O) N-CH (CH3) -CH3, C (O) NCH2-CH2-CH3, AMONG OTHERS; R1 'IS HALOGEN, C1-4 ALKYL SUBSTITUTED OR NOT WITH HALO. CYANO, NITRO, AMONG OTHERS; G1 AND G2 ARE INDEPENDENTLY NITROGEN; G3 IS NH; R3 IS PHENYL OPTIONALLY REPLACED ONE OR MORE TIMES WITH HALOGEN, NITRO, AMONG OTHERS. PREFERRED COMPOUNDS ARE: 3- [2- (4-AMINO-1-PIPERIDINYL) -8- (2,6-DIFLUOROPHENYL) -7-OXO-5,6,7,8-TETRAHYDROPYRIMIDO [4,5-d] PYRIMIDIN -4-IL] -N-CYCLOBUTYL-4-METHYLBENZAMIDE; 3- {8- (2,6-DIFLUOROPHENYL) -2 - [[3- (DIMETHYLAMINO) PROPYL] (METHYL) AMINO] -7-OXO-5,6,7,8-TETRAHYDROPYRIMIDO [4,5-d] PYRIMIDIN-4-IL} -4-METHYL-N- (PHENYLMETIL) BENZAMIDE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF CSBP / p38 / RK KINASES USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES

PE2010000198A 2005-03-25 2006-03-23 COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38 PE20100741A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66534705P 2005-03-25 2005-03-25

Publications (1)

Publication Number Publication Date
PE20100741A1 true PE20100741A1 (en) 2010-11-25

Family

ID=37053936

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2006000331A PE20061193A1 (en) 2005-03-25 2006-03-23 DERIVATIVES OF 3,4-DIHYDROPYRIMIDO [4,5-d] PYRIMIDIN-2- [1H] -0NA AS KINASE INHIBITORS p38
PE2010000198A PE20100741A1 (en) 2005-03-25 2006-03-23 COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2006000331A PE20061193A1 (en) 2005-03-25 2006-03-23 DERIVATIVES OF 3,4-DIHYDROPYRIMIDO [4,5-d] PYRIMIDIN-2- [1H] -0NA AS KINASE INHIBITORS p38

Country Status (23)

Country Link
US (4) US7674789B2 (en)
EP (1) EP1866311A4 (en)
JP (1) JP2008535820A (en)
KR (1) KR20080005223A (en)
CN (1) CN101184758B (en)
AP (1) AP2281A (en)
AR (1) AR053450A1 (en)
AU (1) AU2006229967B2 (en)
BR (1) BRPI0609579A2 (en)
CA (1) CA2602546A1 (en)
EA (1) EA200702074A1 (en)
IL (1) IL185915A0 (en)
MA (1) MA29340B1 (en)
MX (1) MX2007011883A (en)
NO (1) NO20075273L (en)
NZ (1) NZ561438A (en)
PE (2) PE20061193A1 (en)
SG (1) SG166100A1 (en)
TW (1) TW200724142A (en)
UA (1) UA95230C2 (en)
UY (1) UY29439A1 (en)
WO (1) WO2006104889A2 (en)
ZA (1) ZA200707798B (en)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
AU2002246855B2 (en) 2000-10-23 2005-12-22 Smithkline Beecham Corporation Novel compounds
ATE375980T1 (en) 2002-02-12 2007-11-15 Smithkline Beecham Corp NICOTINAMIDES AND THEIR USE AS P38 INHIBITORS
ATE370952T1 (en) * 2002-04-19 2007-09-15 Smithkline Beecham Corp NEW CONNECTIONS
WO2006104917A2 (en) * 2005-03-25 2006-10-05 Glaxo Group Limited Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1h)-one derivatives
JP2008535822A (en) * 2005-03-25 2008-09-04 グラクソ グループ リミテッド New compounds
TW200724142A (en) * 2005-03-25 2007-07-01 Glaxo Group Ltd Novel compounds
AR053346A1 (en) 2005-03-25 2007-05-02 Glaxo Group Ltd COMPOSITE DERIVED FROM 8H -PIRIDO (2,3-D) PIRIMIDIN -7 ONA 2,4,8- TRISUSTITUTED PHARMACEUTICAL COMPOSITION AND USE TO PREPARE A COMPOSITION FOR TREATMENT AND PROFILXIS OF A DISEASE MEDIATED BY KINASE CSBP / RK / P38
WO2007147103A2 (en) * 2006-06-16 2007-12-21 Glaxo Group Limited Novel compounds
WO2007147104A2 (en) * 2006-06-16 2007-12-21 Glaxo Group Limited Novel compounds
JP2009542818A (en) * 2006-06-16 2009-12-03 グラクソ グループ リミテッド New compounds
EP2114885B1 (en) * 2007-02-09 2016-01-27 Dow AgroSciences LLC Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
JP2011524365A (en) * 2008-06-11 2011-09-01 アイアールエム・リミテッド・ライアビリティ・カンパニー Compounds and compositions useful for the treatment of malaria
CN103827118B (en) * 2011-07-27 2016-03-09 葛兰素集团有限公司 Bicyclic pyrimidin ketone compound
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
CA3128468A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
CN111961034A (en) * 2019-05-20 2020-11-20 浙江同源康医药股份有限公司 Compounds useful as RET kinase inhibitors and uses thereof
CN113750095B (en) * 2021-03-10 2023-07-04 中国医学科学院医药生物技术研究所 Application of compound containing cyclopropyl skeleton in preparation of medicines for treating and/or preventing coronavirus infection

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA966134A (en) * 1972-05-05 1975-04-15 Haydn W.R. Williams 1,8-naphthyridine compounds
ZA803539B (en) * 1979-06-14 1982-01-27 Wellcome Found Alkoxybenzylrimidines method for their preparation formulation thereof and their use in medicine
CY1308A (en) 1979-12-06 1985-12-06 Glaxo Group Ltd Device for dispensing medicaments
US4353656A (en) 1980-10-14 1982-10-12 Xerox Corporation Moving coil, multiple energy print hammer system including a closed loop servo
ATE23272T1 (en) 1981-07-08 1986-11-15 Draco Ab POWDER INHALER.
WO1983002613A1 (en) 1981-07-20 1983-08-04 Sallmann, Alfred Trisubstituted oxazo compounds
GB2169265B (en) 1982-10-08 1987-08-12 Glaxo Group Ltd Pack for medicament
US4778054A (en) 1982-10-08 1988-10-18 Glaxo Group Limited Pack for administering medicaments to patients
NZ205892A (en) 1982-10-08 1987-07-31 Glaxo Group Ltd Inhalation device; including a penetrating member and rotatable indexing means
JPS60226882A (en) * 1984-04-24 1985-11-12 Nippon Zoki Pharmaceut Co Ltd Novel pyrimidopyrimidine derivative
US4560691A (en) * 1984-07-13 1985-12-24 Sterling Drug Inc. 5-(Phenyl)-1,6-naphthyridin-2(1H)-ones, their cardiotonic use and preparation
PT83094B (en) 1985-07-30 1993-07-30 Glaxo Group Ltd DEVICES PROPER FOR THE ADMINISTRATION OF MEDICINES TO PATIENTS
EP0278686A1 (en) 1987-02-07 1988-08-17 The Wellcome Foundation Limited Pyridopyrimidines methods for their preparation and pharmaceutical formulations thereof
JPH01261306A (en) 1988-04-13 1989-10-18 Nippon Kayaku Co Ltd Flowering promoter comprising 2-alkylthio-4-aminopyrimidine derivative as active ingredient
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
IE913473A1 (en) * 1990-10-15 1992-04-22 Fujisawa Pharmaceutical Co Quinazoline derivatives and their preparation
WO1992012154A1 (en) 1990-12-31 1992-07-23 Fujisawa Pharmaceutical Co., Ltd. Imidazotriazine derivatives
AU658646B2 (en) * 1991-05-10 1995-04-27 Rhone-Poulenc Rorer International (Holdings) Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
IL102764A0 (en) 1991-08-16 1993-01-31 Merck & Co Inc Quinazoline derivatives,and pharmaceutical compositions containing them
DE4131029A1 (en) * 1991-09-18 1993-07-29 Basf Ag SUBSTITUTED PYRIDO (2,3-D) PYRIMIDINE AS ANTIDOTS
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
GB9303993D0 (en) 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
US5466692A (en) * 1993-03-24 1995-11-14 American Home Products Corporation Substituted pyridopyrimidines and antihypertensives
US5426110A (en) * 1993-10-06 1995-06-20 Eli Lilly And Company Pyrimidinyl-glutamic acid derivatives
GB9325217D0 (en) 1993-12-09 1994-02-09 Zeneca Ltd Pyrimidine derivatives
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5547954A (en) * 1994-05-26 1996-08-20 Fmc Corporation 2,4-Diamino-5,6-disubstituted-and 5,6,7-trisubstituted-5-deazapteridines as insecticides
TW574214B (en) 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
NZ289157A (en) 1994-06-15 1998-03-25 Wellcome Found Amidino sulphoxides and sulphones; medicaments for selective inhibition of inducible nitric oxide synthase
WO1996006843A1 (en) * 1994-08-29 1996-03-07 Yamanouchi Pharmaceutical Co., Ltd. Novel naphthyridine derivative and medicinal composition thereof
IL115256A0 (en) * 1994-11-14 1995-12-31 Warner Lambert Co 6-Aryl pyrido (2,3-d) pyrimidines and naphthyridines and their use
US5772085A (en) 1995-03-10 1998-06-30 Minnesota Mining And Manufacturing Free flow aerosol valves
US5620981A (en) * 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
US5760220A (en) * 1995-06-07 1998-06-02 American Home Products Corporation Process for preparation of biphenyl derivatives
US5767097A (en) * 1996-01-23 1998-06-16 Icn Pharmaceuticals, Inc. Specific modulation of Th1/Th2 cytokine expression by ribavirin in activated T-lymphocytes
JP2001511764A (en) 1996-04-12 2001-08-14 住友製薬株式会社 Piperidinyl pyrimidine derivative
US6875769B2 (en) * 1996-05-23 2005-04-05 Pfizer Inc. Substituted6,6-hetero-bicyclicderivatives
ZA973884B (en) * 1996-05-23 1998-11-06 Du Pont Merck Pharma Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders
NZ333727A (en) * 1996-08-06 2000-09-29 Pfizer Substituted pyrido- or pyrimido-containing 6,6- or 6,7-bicyclic arylsulfonylamino hydroxamic acid derivatives
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
US6509320B1 (en) * 1996-10-16 2003-01-21 Icn Pharmaceuticals, Inc. Purine L-nucleosides, analogs and uses thereof
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
GB9700226D0 (en) 1997-01-08 1997-02-26 Glaxo Group Ltd Inhalation device
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
AU749750B2 (en) 1997-02-05 2002-07-04 Warner-Lambert Company Pyrido {2,3-d} pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
US5945422A (en) * 1997-02-05 1999-08-31 Warner-Lambert Company N-oxides of amino containing pyrido 2,3-D! pyrimidines
US6498163B1 (en) * 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
DE19723722A1 (en) 1997-05-30 1998-12-10 Schering Ag Nonsteroidal progestogens
AR017219A1 (en) 1997-12-19 2001-08-22 Smithkline Beecham Corp IMIDAZOL DERIVATIVES 1,4,5 SUBSTITUTES, COMPOSITIONS THAT INCLUDE THEM, PROCEDURE FOR THE PREPARATION OF SUCH DERIVATIVES, USE OF DERIVATIVES TO MANUFACTURE OF A MEDICINAL PRODUCT
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
BR9908004A (en) * 1998-02-17 2001-12-18 Tularik Inc Compound, composition and method for preventing or suppressing a viral infection
JP2000038350A (en) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd Diabetes therapeutic drug
DE69939168D1 (en) 1998-05-26 2008-09-04 Warner Lambert Co BICYCLIC PYRIMIDINES AND BICYCLIC 3,4-DIHYDROPYRIMIDINES AS INHIBITORS OF CELL REPRODUCTION
US6248225B1 (en) * 1998-05-26 2001-06-19 Ppg Industries Ohio, Inc. Process for forming a two-coat electrodeposited composite coating the composite coating and chip resistant electrodeposited coating composition
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
WO1999064400A1 (en) * 1998-06-12 1999-12-16 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
ATE232205T1 (en) * 1998-10-01 2003-02-15 Astrazeneca Ab QUINOLINE AND QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS OF DISEASES INVOLVING CYTOKINE
WO2000023444A1 (en) 1998-10-21 2000-04-27 Abbott Laboratories 5,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
US6358959B1 (en) 1999-01-26 2002-03-19 Merck & Co., Inc. Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
WO2000066590A2 (en) 1999-05-04 2000-11-09 Ligand Pharmaceuticals, Inc. Tetracyclic progesterone receptor modulator compounds and methods
CO5180649A1 (en) 1999-09-01 2002-07-30 Abbott Lab ANTAGONISTS OF GLUCOCORTICOID RECEPTORS FOR THE TREATMENT OF DIABETES FOR THE TREATMENT OF DIABETES
SK3792002A3 (en) 1999-09-17 2003-09-11 Abbott Gmbh & Co Kg Kinase inhibitors as therapeutic agents
WO2001042243A2 (en) 1999-12-08 2001-06-14 Advanced Medicine, Inc. Protein kinase inhibitors
US6632666B2 (en) 2000-01-14 2003-10-14 Biolife Solutions, Inc. Normothermic, hypothermic and cryopreservation maintenance and storage of cells, tissues and organs in gel-based media
HUP0204141A3 (en) 2000-01-25 2005-03-29 Warner Lambert Co Pyrido[2,3d]pyrimidine-2,7-diamine inhibitors, pharmaceutical compositions containing them and their use
HUP0203803A3 (en) * 2000-01-27 2004-09-28 Warner Lambert Co Pyridopyrimidinone derivatives for treatment of neurodegenerative disease
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
NZ520962A (en) 2000-03-06 2003-09-26 Warner Lambert Co 5-alkylpyrido[2,3-d]pyrimidines cyclin-dependent tyrosine kinase inhibitors
WO2002008948A2 (en) * 2000-07-24 2002-01-31 Vivcom, Inc. System and method for indexing, searching, identifying, and editing portions of electronic multimedia files
KR20030031198A (en) 2000-09-29 2003-04-18 글락소 그룹 리미티드 Morpholin-acetamide derivatives for the treatment of inflammatory diseases
WO2002060869A2 (en) 2000-10-19 2002-08-08 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
AU2002246855B2 (en) * 2000-10-23 2005-12-22 Smithkline Beecham Corporation Novel compounds
AU2002246677B2 (en) 2000-12-20 2006-11-16 Merck Sharp & Dohme Corp. (Halo-Benzo Carbonyl)Heterocyclo Fused Phenyl p38 Kinase Inhibiting Agents
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
PE20030008A1 (en) 2001-06-19 2003-01-22 Bristol Myers Squibb Co DUAL INHIBITORS OF PDE 7 AND PDE 4
WO2003010143A1 (en) 2001-07-26 2003-02-06 Samsung Electronics Co., Ltd. Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses
JP4178783B2 (en) 2001-10-19 2008-11-12 三菱化学株式会社 Optical recording medium
US7019002B2 (en) * 2001-12-11 2006-03-28 Pharmacia & Upjohn, S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2003059899A1 (en) 2002-01-14 2003-07-24 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
US6831093B2 (en) 2002-01-22 2004-12-14 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
CA2473026C (en) * 2002-01-22 2011-05-03 Warner-Lambert Company Llc 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
EP1490062B1 (en) 2002-03-26 2007-12-19 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2003230700A1 (en) 2002-03-26 2003-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (en) 2002-04-02 2003-12-18 Schering Ag Quinoline and isoquinoline derivatives, a pharmaceutical agent and their use as anti-inflammatory agents
DE60335869D1 (en) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1H-BENZO (F) INDAZOL-5-YL DERIVATIVES AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS
US20040063658A1 (en) * 2002-05-06 2004-04-01 Roberts Christopher Don Nucleoside derivatives for treating hepatitis C virus infection
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
CA2491994C (en) 2002-07-08 2013-11-05 Pfizer Products Inc. Modulators of the glucocorticoid receptor
ATE456100T1 (en) 2002-07-18 2010-02-15 Bristol Myers Squibb Co COMPOSITIONS AND METHODS RELATED TO THE NUCLEAR HORMONE RECEPTOR SITE II
PL375442A1 (en) 2002-07-18 2005-11-28 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2003270783C1 (en) 2002-09-20 2010-05-20 Merck Sharp & Dohme Corp. Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
WO2004043367A2 (en) * 2002-11-06 2004-05-27 Bristol-Myers Squibb Company Fused heterocyclic compounds and use thereof
JP2004203751A (en) 2002-12-24 2004-07-22 Pfizer Inc Substituted 6,6-heterobicyclic derivatives
BRPI0406809A (en) * 2003-01-17 2005-12-27 Warner Lambert Co 2-Aminopyridine substituted heterocycles as cell proliferation inhibitors
CA2515939A1 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Novel compounds
US7138412B2 (en) * 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
EP1636195A1 (en) * 2003-05-27 2006-03-22 Pfizer Products Inc. Quinazolines and pyrido[3,4-d]pyrimidines as receptor tyrosine kinase inhibitors
TWI220897B (en) * 2003-07-22 2004-09-11 Benq Corp Recording media feeding system and method
US7968545B2 (en) 2003-08-05 2011-06-28 Vertex Pharmaceuticals Inc. Compositions useful as inhibitors of voltage-gated ion channels
US7098222B2 (en) * 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
WO2006039469A1 (en) * 2004-09-29 2006-04-13 Graphic Packaging International, Inc Carton with dispenser having access features
EP1828186A1 (en) * 2004-12-13 2007-09-05 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
TW200724142A (en) * 2005-03-25 2007-07-01 Glaxo Group Ltd Novel compounds
AR053346A1 (en) * 2005-03-25 2007-05-02 Glaxo Group Ltd COMPOSITE DERIVED FROM 8H -PIRIDO (2,3-D) PIRIMIDIN -7 ONA 2,4,8- TRISUSTITUTED PHARMACEUTICAL COMPOSITION AND USE TO PREPARE A COMPOSITION FOR TREATMENT AND PROFILXIS OF A DISEASE MEDIATED BY KINASE CSBP / RK / P38
JP2008535822A (en) * 2005-03-25 2008-09-04 グラクソ グループ リミテッド New compounds
WO2006104917A2 (en) * 2005-03-25 2006-10-05 Glaxo Group Limited Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1h)-one derivatives

Also Published As

Publication number Publication date
AP2007004171A0 (en) 2007-10-31
SG166100A1 (en) 2010-11-29
BRPI0609579A2 (en) 2010-04-20
MX2007011883A (en) 2007-11-13
NO20075273L (en) 2007-12-12
CN101184758A (en) 2008-05-21
AP2281A (en) 2011-10-31
AR053450A1 (en) 2007-05-09
CN101184758B (en) 2012-05-02
MA29340B1 (en) 2008-03-03
WO2006104889A3 (en) 2007-04-12
AU2006229967A1 (en) 2006-10-05
PE20061193A1 (en) 2006-12-02
EP1866311A2 (en) 2007-12-19
IL185915A0 (en) 2008-01-06
US20090239846A1 (en) 2009-09-24
AU2006229967B2 (en) 2012-02-09
US20100093766A1 (en) 2010-04-15
JP2008535820A (en) 2008-09-04
CA2602546A1 (en) 2006-10-05
WO2006104889A2 (en) 2006-10-05
UY29439A1 (en) 2006-10-02
EA200702074A1 (en) 2008-02-28
KR20080005223A (en) 2008-01-10
TW200724142A (en) 2007-07-01
UA95230C2 (en) 2011-07-25
ZA200707798B (en) 2009-08-26
US20060235030A1 (en) 2006-10-19
US20100093765A1 (en) 2010-04-15
US7674789B2 (en) 2010-03-09
NZ561438A (en) 2011-02-25
EP1866311A4 (en) 2010-03-31

Similar Documents

Publication Publication Date Title
PE20100741A1 (en) COMPOUNDS DERIVED FROM 3,4-DIHYDROPYRIMIDE [4,5-d] PYRIMIDIN-2 (1H) -ONE AS KINASE INHIBITORS p38
PE20110944A1 (en) PYRAZOLO [3,4-d] PYRIMIDINE DERIVATIVES AS PDE1 INHIBITORS
PE20100737A1 (en) NEW COMPOUNDS
PE20120121A1 (en) IMIDAZOPYRAZINE DERIVATIVES AS SYK INHIBITORS
PE20140390A1 (en) DERIVATIVES OF IMIDAZO [1,2-B] PYRIDAZINE AND IMIDAZO [4,5-B] PYRIDINE AS JAK INHIBITORS
PE20091408A1 (en) COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS
PE20120120A1 (en) DERIVATIVES OF 2H-PYRAZOLO [3,4-d] PYRIMIDINE-4,6 (5H, 7H) -DIONA, AS PDE1 INHIBITORS
PE20030129A1 (en) IMIDAZOTRIAZINES
PE20120814A1 (en) COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
PE20080315A1 (en) DERIVATIVES OF PIRAZOLO- [3,4-d] -PYRIMIDINES AS INHIBITORS OF KINASE PI-3
PE20010760A1 (en) DERIVATIVES OF DIHYDROPYRIMIDE [4,5] PYRIMIDINONE ALKYLAMINE SUBSTITUTED AS INHIBITORS OF KINASES p38
PE20061067A1 (en) PYRIMIDINE DERIVATIVES
PE20080548A1 (en) DERIVATIVES OF [4,5 '] BIPYRIMIDINYL-6,4'-DIAMINE AS PROTEIN KINASE INHIBITORS
PE20141700A1 (en) 2- (2,4,5-ANILINE SUBSTITUTED) PYRIMIDINE COMPOUNDS
PE20090279A1 (en) DERIVATIVES OF 3,3-SPYROINDOLINONE AS ANTAGONISTS AGENTS OF MDM2
PE20090944A1 (en) BICYCLE PYRIMIDINES FUSED AS INHIBITORS OF THE PI3K / AKT VIA
PE20060586A1 (en) PYRAZOLO [1,5-a] PYRIMIDINE DERIVATIVES AS ANTAGONISTS OF THE CRF RECEPTOR
PE20050681A1 (en) PYRID [2,3-d] PYRIMIDINE-2,4-DIAMINES AS INHIBITORS OF PDE 2
PE20090718A1 (en) SPIROINDOLINONE DERIVATIVES
PE20010629A1 (en) TRIAZOLPYRIDINAMINE DERIVATIVES AS ADENOSINE RECEPTOR LINKS
PE20060185A1 (en) ADENOSINE A2A RECEPTOR ANTAGONIST WITH PYRAZOLE STRUCTURE - [4,3-e] -1,2,4-TRIAZOLO- [1,5-c] -PYRIMIDINE
PE20090370A1 (en) DERIVATIVES OF FUSED HETEROCYCLE AS KINASE INHIBITORS
PE20210658A1 (en) TRIAZOLOPYRIMIDINE DERIVATIVES FOR USE AS GHRELIN O-ACILTRANSFERASE (GOAT) INHIBITORS
PE20120534A1 (en) PYRIMIDINES FUSED AS INHIBITORS OF Akt
PE20081159A1 (en) INHIBITORS OF KINASES AND METHODS FOR THEIR USE

Legal Events

Date Code Title Description
FD Application declared void or lapsed